Pyrus ussuriensis Maxim. leaves extract ameliorates DNCB-induced atopic dermatitis-like symptoms in NC/Nga mice.

PURPOSE: Pyrus ussuriensis Maxim. has been reported to treat the fever, cough, asthma, and chronic skin disease in Korean Medicine. However, there is no scientific evidence for the use of Pyrus ussuriensis Maxim. Leaves (PUL) extract or its mechanism of action in atopic dermatitis (AD). This study was performed to find the potential therapeutic effects of PUL on the progression of AD using in vitro and in vivo experimental models. METHODS: We examined the effects of PUL on the production of nitric oxide (NO) in RAW 264.7, Interleukin 6 (IL-6) and Interleukin 1ß (IL-1ß) in tumor necrosis factor α (TNF-α) -induced HaCaT cells, respectively. The PUL extract was topically administered to the 2,4-Dinitrochlorobenzene (DNCB) -treated NC/Nga mice. The potential effects of PUL extract were evaluated by measuring the dermatitis score, scratching behavior and serum levels of immunoglobulin E (IgE). The Interleukin 4 (IL-4) and Interleukin 13 (IL-13) cytokines levels were also measured in the splenocytes. In addition, the major components from PUL were analyzed using high performance liquid chromatography (HPLC). RESULTS: PUL extract significantly reduced the level of NO in RAW 264.7 cells, as well as IL-6 and IL-1ß in TNF-α-induced HaCaT cells. It also reduced IL-4 and IL-13 levels in splenocytes. In DNCB-treated NC/Nga mice, PUL extract significantly ameliorated the dermatitis severity, scratching tendency and transepidermal water loss (TEWL) compared to the negative control. Also, it normalized skin barriers with decreased production of IgE in mice serum. The arbutin, chlorogenic acid, and rutin were identified as major constituents of the extract by HPLC analysis. These constituents may be involved either alone or together in the regulation of atopic dermatitis. CONCLUSION: Our studies indicate that PUL ameliorates atopic dermatitis-like symptoms by suppressing the proinflammatory cytokines and immune stimuli in both in vitro and in vivo animal models. Therefore, these data suggest that PUL might be an effective natural resource for the treatment of AD.

Novel Polymer-Free Everolimus-Eluting Stent Fabricated using Femtosecond Laser Improves Re-endothelialization and Anti-inflammation.

The aim of this study was to fabricate a novel polymer-free everolimus-eluting stent with nanostructure using a femtosecond laser (FSL). The stent were coated with everolimus (EVL) using FSL and electrospinning processes. The surface was rendered hydrophobic, which negatively affected both platelet adhesion (82.1%) and smooth muscle cell response. Animal study was performed using a porcine coronary restenosis model. The study groups were divided into 1) bare metal stent (BMS), 2) poly(L-lactide) (PLA)-based EVL drug eluting stent (DES), 3) commercial EVL-eluting DES, and 4) FSL-EVL-DES. After four weeks of stent implantation, various analyses were performed. Quantitative analysis showed that the amount of in-stent restenosis was higher in the BMS group (BMS; 27.8 ± 2.68%, PLA-based DES; 12.2 ± 0.57%, commercial DES; 9.8 ± 0.28%, and FSL-DES; 9.3 ± 0.25%, n = 10, p < 0.05). Specifically, the inflammation score was reduced in the FSL-DES group (1.9 ± 0.39, n = 10, p < 0.05). The increment in re-endothelialization in the FSL-DES group was confirmed by immunofluorescence analysis. Taken together, the novel polymer-free EVL-eluting stent fabricated using FSL can be an innovative DES with reduced risk of ISR, thrombosis, and inflammation.

Metabolism and antioxidant effect of malaxinic acid and its corresponding aglycone in rat blood plasma.

Malaxinic acid (MA) is a phenolic acid compound, found mainly in pear fruits (Pyrus pyrifolia N.), that is isoprenylated on the C-3 position of benzoic acid. Recently, the effects of prenylated phenolics on health have received much interest owing to their reported potent beneficial biological effects. We conducted a comparative study in rats to determine the metabolism, pharmacokinetics, and antioxidative activities of MA and its corresponding aglycone (MAA). MA and MAA were orally administered to rats (Sprague-Dawley, male, 6 weeks old) and their metabolites in plasma were analyzed. In addition, the MA metabolites in plasma were separated and the structures were confirmed via NMR and HR-MS analyses. The antioxidative activities of MA and MAA were evaluated by measuring their inhibitory effects on the 2,2'-azobis(2-amidinopropane)dihydrochloride- or copper ion-induced lipid peroxidation of rat plasma. MA was not absorbed in the intact form (the glucoside); both MA and MAA were absorbed as MAA and its metabolite form (glucuronide or sulfate). Moreover, the observed metabolite was the glucuronate of MAA rather than the glucuronide or sulfate. Concentrations of the free form of aglycone (MA administration, 4.6 ± 2.2µM; MAA administration, 7.2 ± 2.3µM) and total MAA (MA administration, 19.6 ± 4.4µM; MAA administration, 21.7 ± 3.3µM) in plasma reached a maximum at 15min after the oral administration of MA and MAA, respectively. The relative inhibitory effects on the formation of cholesteryl ester hydroperoxides in plasma collected at 15min after the oral administration of MA, MAA, and p-hydroxybenzoic acid (p-HBA) were as follows: MAA > MA ≥ p-HBA > control. Although the majority of MA and MAA is metabolized to conjugates, the compounds may contribute to the antioxidant defenses in the blood circulation owing to the presence of a phenolic hydroxyl group in the free form.

Phenolics, acyl galactopyranosyl glycerol, and lignan amides from Tetragonia tetragonioides (Pall.) Kuntze.

Eleven antioxidative compounds, including five lignin amides, were isolated from the aerial part of Tetragonia tetragonioides (New Zealand spinach) using 1,1-diphenyl-2-picrylhydrazyl radicalscavenging assay-guided purification. The structures were determined by nuclear magnetic resonance and electrospray ionization-mass spectroscopy. These compounds were identified as methyl linoleate (1), methyl coumarate (2), methyl ferulate (3), 1-O-stearoyl-3-O-ß-D-galactopyranosyl-sn-glycerol (4), 1-O-caffeoyl-ß-D-glucopyranoside (5), N-trans-caffeoyltyramine (6), cannabisin B (7), cannabisin A (8), Ntrans-feruloyltyramine (9), N-cis-feruloyltyramine (10), and N-trans-sinapoyltyramine (11). Compounds 1, 2, 4, 5, and 8-11 were isolated for the first time from this plant.